Trachsel H, Ranu R S, London I M
Proc Natl Acad Sci U S A. 1978 Aug;75(8):3654-8. doi: 10.1073/pnas.75.8.3654.
To define the mechanism of regulation of the protein kinase that is activated in heme deficiency and that inhibits initiation of protein synthesis, we have isolated and purified the heme-reversible form of the protein kinase from rabbit reticulocytes. The inhibitory activity is found in a single band after polyacrylamide gel electrophoresis under nondenaturing conditions. It migrates as a 95,000-dalton polypeptide in 15% sodium dodecyl sulfate/polyacrylamide gels. This purified inhibitor becomes self-phosphorylated in the presence of ATP; the phosphorylated protein and the inhibitory activity copurify. The inhibitor produces characteristic biphasic kinetics of inhibition in reticulocyte lysates and phosphorylates the 38,000-dalton subunit of eukaryotic initiation factor 2 (eIF-2); the inhibition is reversed by added eIF-2. In contrast to the heme-irreversible inhibitor, this heme-reversible inhibitor is no longer inhibitory after incubation with 20 micron hemin. Incubation with hemin also inhibits self-phosphorylation. Preincubation of the heme-reversible inhibitor in the presence of ATP potentiates the inhibition of protein synthesis in the subsequent incubation, as does treatment with N-ethylmaleimide. Phosphorylation of the heme-reversible inhibitor and inhibition of protein synthesis in the lysate due to phosphorylation of eIF-2 appear to be related. These findings suggest that hemin acts directly on the heme-reversible inhibitor.
为了确定在血红素缺乏时被激活并抑制蛋白质合成起始的蛋白激酶的调节机制,我们从兔网织红细胞中分离并纯化了血红素可逆形式的蛋白激酶。在非变性条件下进行聚丙烯酰胺凝胶电泳后,抑制活性出现在单一泳带中。在15%十二烷基硫酸钠/聚丙烯酰胺凝胶中,它以95,000道尔顿的多肽形式迁移。这种纯化的抑制剂在ATP存在下会发生自身磷酸化;磷酸化的蛋白与抑制活性共纯化。该抑制剂在网织红细胞裂解物中产生特征性的双相抑制动力学,并使真核起始因子2(eIF-2)的38,000道尔顿亚基磷酸化;加入eIF-2可逆转这种抑制。与血红素不可逆抑制剂不同,这种血红素可逆抑制剂在与20微摩尔血红素孵育后不再具有抑制作用。与血红素孵育也会抑制自身磷酸化。在ATP存在下对血红素可逆抑制剂进行预孵育会增强随后孵育中对蛋白质合成的抑制作用,用N-乙基马来酰亚胺处理也会如此。血红素可逆抑制剂的磷酸化以及由于eIF-2磷酸化导致裂解物中蛋白质合成的抑制似乎是相关的。这些发现表明血红素直接作用于血红素可逆抑制剂。